产品
编 号:F077039
分子式:C19H17D4ClFNO3
分子量:369.85
产品类型
结构图
CAS No: 1217683-35-6
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产品详情
生物活性:
rel-Paroxetine-d4 (hydrochloride) is an isotope-labeled Paroxetine hydrochloride (HY-B0492). Paroxetine hydrochloride is an orally active and selective serotonin-reuptake inhibitor, commonly prescribed as an GRK2 inhibitor with IC50 of 14?μM. Paroxetine hydrochloride can be used for the research of depressive disorder.
体内研究:
Paroxetine (15 mg/kg/d; p.o.; 15 d) obviously attenuates the symptoms of collagen-induced arthritis (CIA) rats.Animal Model:Collagen-induced arthritis (CIA) model in rats (around 14-day-old)
Dosage:15 mg/kg
Administration:Oral gavage; once daily; 15 days
Result:Helped CIA rats to restore more body weight.
体外研究:
Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs.Paroxetine (1?μM and 10?μM; 4 h) distinctly restrains T cell migration induced by CX3CL1 through inhibiting GRK2. Paroxetine (16 h) inhibits GRK2 induced activation of ERK in splenic T cells.Paroxetine (10 μM) reduces pro-inflammatory cytokines in LPS-stimulated BV2 cells. Paroxetine (0-5 μM) leads to a dose-dependent inhibition on LPS-induced production of TNF-α and IL-1β in BV2 cells. Paroxetine also inhibits lipopolysaccharide (LPS)-induced nitric oxide (NO) production and inducible nitric oxide synthase (iNOS) expression in BV2 cells. Paroxetine (5 μM) blocks LPS-induced JNK activation and attenuates baseline ERK1/2 activity in BV2 cells.Paroxetine relieves microglia-mediated neurotoxicity, and suppresses LPS-stimulated pro-inflammatory cytokines and NO in primary microglial cells.